A state-of-the-art review on LSD1 and its inhibitors in breast cancer: Molecular mechanisms and therapeutic significance

Guan-Jun Yang; Guan-Jun Yang; Guan-Jun Yang; Yan-Jun Liu; Li-Jian Ding; Fan Tao; Ming-Hui Zhu; Zhen-Yuan Shi; Juan-Ming Wen; Meng-Yao Niu; Xiang Li; Zhan-Song Xu; Wan-Jia Qin; Chen-Jie Fei; Chen-Jie Fei; Chen-Jie Fei; Jiong Chen; Jiong Chen; Jiong Chen

doi:10.3389/fphar.2022.989575

Frontiers in Pharmacology (Sep 2022)

A state-of-the-art review on LSD1 and its inhibitors in breast cancer: Molecular mechanisms and therapeutic significance

Guan-Jun Yang,
Guan-Jun Yang,
Guan-Jun Yang,
Yan-Jun Liu,
Li-Jian Ding,
Fan Tao,
Ming-Hui Zhu,
Zhen-Yuan Shi,
Juan-Ming Wen,
Meng-Yao Niu,
Xiang Li,
Zhan-Song Xu,
Wan-Jia Qin,
Chen-Jie Fei,
Chen-Jie Fei,
Chen-Jie Fei,
Jiong Chen,
Jiong Chen,
Jiong Chen

Affiliations

Guan-Jun Yang: State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, Zhejiang, China
Guan-Jun Yang: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Guan-Jun Yang: Key Laboratory of Aquacultural Biotechnology Ministry of Education, Ningbo University, Ningbo, China
Yan-Jun Liu: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Li-Jian Ding: Li Dak Sum Yip Yio Chin Kenneth Li Marine Biopharmaceutical Research Center, Department of Marine Pharmacy, College of Food and Pharmaceutical Sciences, Ningbo University, Ningbo, China
Fan Tao: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Ming-Hui Zhu: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Zhen-Yuan Shi: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Juan-Ming Wen: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Meng-Yao Niu: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Xiang Li: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Zhan-Song Xu: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Wan-Jia Qin: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Chen-Jie Fei: State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, Zhejiang, China
Chen-Jie Fei: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Chen-Jie Fei: Key Laboratory of Aquacultural Biotechnology Ministry of Education, Ningbo University, Ningbo, China
Jiong Chen: State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, Zhejiang, China
Jiong Chen: Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, China
Jiong Chen: Key Laboratory of Aquacultural Biotechnology Ministry of Education, Ningbo University, Ningbo, China

DOI: https://doi.org/10.3389/fphar.2022.989575
Journal volume & issue: Vol. 13

Abstract

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Breast cancer (BC) is a kind of malignant cancer in women, and it has become the most diagnosed cancer worldwide since 2020. Histone methylation is a common biological epigenetic modification mediating varieties of physiological and pathological processes. Lysine-specific demethylase 1 (LSD1), a first identified histone demethylase, mediates the removal of methyl groups from histones H3K4me1/2 and H3K9me1/2 and plays a crucial role in varieties of cancer progression. It is also specifically amplified in breast cancer and contributes to BC tumorigenesis and drug resistance via both demethylase and non-demethylase manners. This review will provide insight into the overview structure of LSD1, summarize its action mechanisms in BC, describe the therapeutic potential of LSD1 inhibitors in BC, and prospect the current opportunities and challenges of targeting LSD1 for BC therapy.

Published in Frontiers in Pharmacology

ISSN: 1663-9812 (Online)
Publisher: Frontiers Media S.A.
Country of publisher: Switzerland
LCC subjects: Medicine: Therapeutics. Pharmacology
Website: http://journal.frontiersin.org/journals/pharmacology

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